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Biological activities of the product obtained from the reaction of 2-chloro-N-(pyridin-2-yl)acetamide with 5-fluorouracil

Authors

Shirin Azimboyeva, Burieva Dilnoza Madarttovna, Yusufov Mukhriddin Saidovich, Bobonazarova Sarvinoz Habibullaevna, Abdushukurov Anvar Kabirovich

Rubric:Chemistry
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Annotation

The chloroacetylation reaction of 2-aminopyridine derivatives was carried out, and the compound synthesized based on the reactions of the obtained chloroacetyl products with 5-fluorouracil was evaluated using the PASS Online program, which predicts the biological activity spectrum of substances based on their structure. When tested against various cancer and normal cell lines, the candidate compound demonstrated high efficacy against leukemia (Kasumi-1) and certain tumors of epithelial origin. At the same time, low activity observed in normal fibroblast cells indicates that the compound possesses selective activity and may potentially exhibit low toxicity. The antibacterial activity of the planned compound was also evaluated, showing the highest activity against Enterococcus faecalis ATCC 29212 and Mycobacterium tuberculosis H37Rv. The drug-like properties and possible adverse effects of the compound were further analyzed using the PASS program.

Keywords

cancer cells
2-aminopyridine
5-fluorouracil
PASS Online
tuberculosis bacteria

Authors

Shirin Azimboyeva, Burieva Dilnoza Madarttovna, Yusufov Mukhriddin Saidovich, Bobonazarova Sarvinoz Habibullaevna, Abdushukurov Anvar Kabirovich

References:

Pozharskii AF, Soldatenkov AT, Katritzky AR. Heterocycles in life and society: an introduction to heterocyclic chemistry, biochemistry and applications. 2nd ed. Chichester: John Wiley & Sons; 2011.

 Grahman PL. An introduction to medicinal chemistry. 2nd ed. Oxford: Oxford University Press; 2001.

Silverman RB, The organic chemistry of drug design and drug action. London: Academic Press; 1992.

a. World Health Organization Tuberculosis Programme. Available from: Global tuberculosis report 2015/WHO/ http://www.who.int/tb/ publications/global_report/en/ [last accessed 19 Feb 2016]. b. http://www.who.int/mediacentre/factsheets/fs297/en/ [last accessed 19 Feb 2016].

Rescifina A, Zagni C, Varrica MG, et al. Recent advances in small organic molecules as DNA intercalating agents: synthesis, activity, and modeling. Eur J Med Chem 2014;74:95–115.

 Xiang P, Zhou T, Wang L, et al. Novel benzothiazole, benzimidazolee and benzoxazole derivatives as potential antitumor agents: synthesis and preliminary in vitro biological evaluation. Molecules 2012;17:873–83.

Wissner A, Mansour TS. The development of HKI-272 and related compounds for the treatment of cancer. Arch Pharm 2008;341: 465–77.

Zbancioc AM, Zbancioc G, Tanase C, et al. Design, synthesis and in vitro anticancer activity of a new class of bifunctional DNA intercalators. Lett Drug Des Discov 2010;7:644–9.

Luca MC, Tura V, Mangalagiu II. Considerations concerning design and mechanism of action of a new class of anticancer dual DNA intercalators. Med Hypotheses 2010;75:627–9.

Koseki Y, Kinjo T, Kobayashi M, Aoki S. Identification of novel antimycobacterial chemical agents through the in silico multi-conformational structure-based drug screening of a largescale chemical library. Eur J Med Chem 2013;60:333–9.

Gising J, Nilsson MT, Odell LR, et al. Trisubstituted imidazoles as Mycobacterium tuberculosis glutamine synthetase inhibitors. J Med Chem 2012;55:2894–8.

Villemagne B, Crauste C, Flipo M, et al. Tuberculosis: the drug development pipeline at a glance. Eur J Med Chem 2012;51:1–16.

Pandey J, Tiwari VK, Verma SS, et al. Synthesis and antitubercular screening of imidazole derivatives. Eur J Med Chem 2009;44: 3350–5.

Danac R, Managalagiu II. Antimycobacterial activity of nitrogen heterocycles derivatives: bipyridine derivatives. Part III. Eur J Med Chem 2014;74:664–70.

Bobonazarova S. et al. 2-{[(1S, 2S)-1-Hydroxy-1-phenylpropan-2-yl](methyl) amino}-N-(3-methylphenyl) acetamide //IUCrData. – 2025. – Vol. 10. – №. 7. – P. x250578.

Habibullaevna B. S. et al. Reactions of n-chloracetylation of toluidine isomers //Austrian Journal of Technical and Natural Sciences. – 2024. – №. 3-4. – С. 12-16.

 Ochilov S. H. et al. Synthesis of a new derivative of 5-fluorouracil based on 2-chloro-N-(4-iodophenyl) acetamide and study of its biological activity against cancer cells //Austrian journal of technical and natural sciences. – P. 14-18.

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